《Design, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors》 was written by Shu, Lei; Chen, Chengjuan; Huan, Xueting; Huang, Hao; Wang, Manman; Zhang, Jianqiu; Yan, Yile; Liu, Jianming; Zhang, Tiantai; Zhang, Dayong. Application In Synthesis of 4,6-Dichloropyrimidine And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:
In this work, poorly selective compounds based on 4- or 6-phenyl-pyrimidine derivatives I and II [R = H, prop-2-enamidyl, but-2-enamidyl, 2-cyanoacetamidyl; R1 = 1-methyl-1H-pyrazol-4-yl, 1-(2-methoxyethyl)-1H-pyrazol-4-yl, 4-(4-morpholinyl)phenyl, etc.; R2 = H, prop-2-enamidyl, but-2-enamidyl, 2-cyanoacetamidyl] have been improved to highly potent and selective compounds by designing a covalent binding tether, which attaches to the unique cysteine (Cys909) residue in JAK3. Compound II [R = prop-2-enamidyl; R1 = 4-(4-morpholinyl)phenyl, R2 = H (A)] exhibited potent JAK3 inhibitory activity (IC50 = 1.7 nM) with an excellent selectivity profile when compared to the other JAK isoforms (>588-fold). In a cellular assay, compound (A) strongly inhibited JAK3-dependent signaling and T cell proliferation. Moreover, in vivo data revealed that compound (A) significantly suppressed oxazolone (OXZ)-induced delayed hypersensitivity responses in Balb/c mice. Compound (A) also displayed decent pharmacokinetic properties and was suitable for in vivo use. Taken together, these results indicated that compound (A) may be a promising tool compound as a selective JAK3 inhibitor for treating autoimmune diseases. The experimental process involved the reaction of 4,6-Dichloropyrimidine(cas: 1193-21-1Application In Synthesis of 4,6-Dichloropyrimidine)
4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Application In Synthesis of 4,6-Dichloropyrimidine
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia